Harman Patil (Editor)

Enrofloxacin

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ATCvet code
  
QJ01MA90 (WHO)

Formula
  
C19H22FN3O3

Enrofloxacin

AHFS/Drugs.com
  
International Drug Names

Pregnancy category
  
AU: B3 US: C (Risk not ruled out)

Routes of administration
  
Oral, subcutaneous injection, topical (ear drops)

Legal status
  
AU: S4 (Prescription only) UK: POM (Prescription only)

Bioavailability
  
80% in dogs, 65-75% in sheep

Enrofloxacin


Enrofloxacin (ENR) is a fluoroquinolone antibiotic sold by the Bayer Corporation under the trade name Baytril. Enrofloxacin is currently approved by the FDA for the treatment of individual pets and domestic animals in the United States. In September 2005, the FDA withdrew approval of Baytril for use in water to treat flocks of poultry, as this practice was noted to promote the evolution of fluoroquinolone-resistant strains of the bacterium Campylobacter, a human pathogen.

Contents

It is a bactericidal agent. The bactericidal activity of enrofloxacin is concentration-dependent, with susceptible bacteria cell death occurring within 20–30 minutes of exposure. Enrofloxacin has demonstrated a significant post-antibiotic effect for both Gram-negative and Gram-positive bacteria and is active in both stationary and growth phases of bacterial replication. Enrofloxacin is partially deethylated by CYP450 into the active metabolite ciprofloxacin, which is also a fluoroquinolone antibiotic, used preferentially in humans.

Activity and susceptibility data

Enrofloxacin is a synthetic antibacterial agent from the class of the fluoroquinolone carboxylic acid derivatives. It has antibacterial activity against a broad spectrum of Gram-negative and Gram-positive bacteria. Its mechanism of action is not thoroughly understood, but it is believed to act by inhibiting bacterial DNA gyrase (a type-II topoisomerase), thereby preventing DNA supercoiling and DNA synthesis. It is effective against:

  • Pseudomonas aeruginosa
  • Klebsiella
  • Escherichia coli
  • Enterobacter
  • Campylobacter
  • Shigella
  • Salmonella
  • Aeromonas
  • Haemophilus
  • Proteus
  • Yersinia
  • Serratia
  • Vibrio
  • Brucella
  • Chlamydia trachomatis
  • Staphylococcus (including penicillinase-producing and methicillin-resistant strains)
  • Mycoplasma
  • Mycobacterium
  • Variable activity against:

  • Streptococcus
  • Ineffective against:

  • Anaerobes
  • The following data represent minimum inhibitory concentration ranges for a few medically significant bacterial pathogens:

  • Escherichia coli - 0.022 - 0.03 µg/ml
  • Staphylococcus aureus - 0.0925 - 64 µg/ml
  • Pseudomonas aeruginosa - 0.05 µg/ml
  • Contraindications/precautions

    Usage in poultry.

    Adverse effects/warnings

    Enrofloxacin was banned for poultry use in 2005. Baytril should not be used in rapidly growing animals (for example dogs under 12 months - 18 months in large breeds, or kittens under 8 weeks) as it causes abnormalities in the development of articular cartilage.

    Overdosage/acute toxicity

    It is unlikely that an acute overdose of either compound would result in symptoms more serious than either anorexia or vomiting, but the adverse effects noted above could occur. Dogs receiving 10 times the labeled dosage rate of enrofloxacin for at least 14 days developed only vomiting and anorexia. Death did occur in some dogs when fed 25 times the labeled rate for 11 days, however.

  • Oral LD50: greater than 5000 mg/kg
  • Dermal LD50: greater than 2000 mg/kg
  • Inhalation LD50: greater than 3547 mg/m3 (4-hour exposure)
  • Eye effects: irritant; reversible in less than 7 days. In cats, it can produce sudden onset blindness when administered by injection, as it is retinotoxic.
  • Degradation

    The brown rot fungus Gloeophyllum striatum can degrade the fluoroquinolone enrofloxacin using hydroxyl radicals.

    References

    Enrofloxacin Wikipedia